Regorafenib monohydrate

Research use only, not for human use.

A potent multikinase inhibitor that potently inhibits these endothelial cell kinases in biochemical and cellular kinase phosphorylation assays.

A potent multikinase inhibitor that potently inhibits these endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM); inhibits VEGFR1/2/3, PDGFRβ, FGFR1, KIT, RET and B-RAF etc.; exhibits potent dose-dependent TGI in various preclinical human xenograft models in mice; orally active.Colon Cancer Approved.

Regorafenib monohydrate (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells.Regorafenib monohydrate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.Regorafenib monohydrate causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells. Cell Proliferation Assay Cell Line:GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells Concentration:10 μM and 5 nMIncubation Time:96 h Result:Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.Western Blot AnalysisCell Line:NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells Concentration:0, 10, 30, 100, 300, 1000, 3000 nM Incubation Time:30 min Result:Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC50 values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2.

Regorafenib monohydrate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model.Regorafenib monohydrate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model. Animal Model:Rat GS9L glioblastoma xenograft Dosage:10 mg/kg Administration:Orally, single dose or daily for 4 days Result:Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model.Animal Model:Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors Dosage:0, 3, 10, 30, 100 mg/kg Administration:Orally, qd × 9Result:Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation.

BAY 73-4506 monohydrate

Angiogenesis

VEGFR

VEGFR

Cancer

Colon Cancer

1019206-88-2

500.8307

C21H17ClF4N4O4

>98% (HPLC)

10 mM in DMSO

CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F.O

2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, hydrate (1:1)

(-20℃)

With Ice Pack

≥ 2 years